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Imikhiqizo

I-API-Drug Peptide Ziconotide/OMEGA-CGTX MVII A N-type calcium channel blocker

Incazelo emfushane:

I-Ziconotide iwukwenziwa kokwenziwa kwe-hydrophilic polypeptide ω-MVIIA ku-peptide enobuthi be-Pacific fish-eating snail-chicken heart umnenke, futhi iyisidakamizwa sokuqala esisha esingeyona i-opioid esidambisa ubuhlungu esizosetshenziswa emtholampilo.I-Ziconotide ingasetshenziswa njengesidakamizwa esine-opioid analgesic sokuphathwa kwe-intrathecal.


Imininingwane Yomkhiqizo

Omaka bomkhiqizo

Mayelana Nale Nto

Ilungele umjovo we-intrathecal nezinye izindlela zokwelapha (njengama-analgesics e-systemic, i-adjuvant therapy noma i-sheath) i-Ziconotide iyisivimbeli sesiteshi se-calcium esinamandla, esikhethayo futhi esiguqulekayo, esisebenza ngempumelelo ezinhlungwini eziphikisayo, futhi asikhiqizi. ukumelana nezidakamizwa ngemva kokuphathwa isikhathi eside, futhi akubangeli ukuncika ngokomzimba nangokwengqondo, futhi akubangeli ukucindezeleka kokuphefumula okusongela ukuphila ngenxa yokweqisa.Umthamo wansuku zonke onconywayo uncane, unomphumela omuhle wokwelapha, ukuphepha okuphezulu, ukusabela okungekuhle, akukho ukumelana nezidakamizwa kanye nokulutheka.Lo mkhiqizo unethemba elikhulu lemakethe njengesidambisi sezinhlungu.

I-Dispaly yomkhiqizo

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Kungani Khetha Thina

Ngokwezibalo ezingaphelele, izigameko zobuhlungu emhlabeni zingama-35% ~ 45% okwamanje, futhi izigameko zobuhlungu kubantu asebekhulile ziphakeme kakhulu, mayelana ne-75% ~ 90%.Ucwaningo lwaseMelika lubonisa ukuthi izigameko ze-migraine zenyuka zisuka ezigidini ezingu-23.6 ku-1989 zaya ezigidini ezingu-28 ngo-2001. Ekuphenyweni kobuhlungu obungapheli emadolobheni ayisithupha e-China, kutholakala ukuthi isifo sobuhlungu obungapheli kubantu abadala singama-40%, kanti izinga lokwelashwa lingama-35%;Isigameko sobuhlungu obungapheli kubantu asebekhulile singama-65% ~ 80%, kanti izinga lokubona udokotela lingama-85%.Eminyakeni yamuva, izindleko zezokwelapha zokudambisa izinhlungu zikhula unyaka nonyaka.
Kusukela ku-2013 kuya kuJulayi 2015, Isikhungo Sokucwaninga Ngezinhlungu e-United States kanye nezikhungo zezokwelapha eziningana zenze ucwaningo lwesikhathi eside, oluphakathi nendawo kanye nokuhlola umjovo we-intrathecal we-ziconotide ku-93 iziguli ezimhlophe ezikhulile ezimhlophe ezinobuhlungu obukhulu obungapheli.Isilinganiso samaphuzu wedijithali yobuhlungu kanye nesilinganiso sezinzwa sezinzwa zeziguli ezine-injection ye-intrathecal ye-ziconotide futhi ngaphandle komjovo we-ziconotide zaqhathaniswa Phakathi kwabo, iziguli ze-51 zasebenzisa umjovo we-intrathecal we-ziconotide, kuyilapho iziguli ze-42 zingazange.Izibalo eziyisisekelo zobuhlungu zaziyi-7.4 ne-7.9, ngokulandelana.Umthamo onconyiwe womjovo we-intrathecal we-ziconotide wawungu-0.5-2.4 mcg/ ngosuku, owalungiswa ngokuya ngempendulo yobuhlungu besiguli kanye nemiphumela emibi.Umthamo wokuqala ojwayelekile wawuyi-1.6 mcg/ngosuku, u-3.0 mcg/usuku ezinyangeni eziyisi-6 no-2.5 ​​ezinyangeni eziyi-9.Ezinyangeni ezingu-12, bekuyi-1.9 mcg/ ngosuku, futhi ngemva kwezinyanga ezingu-6, izinga lokuncipha lalingu-29.4%, izinga lokukhuphuka elihlukile lalingu-6.4%, futhi izinga lokuthuthukiswa kwezinzwa eziphelele lalingu-69.2% no-35.7% ngokulandelana.Ngemuva kwezinyanga eziyi-12, izinga lokuncipha lalingama-34.4% no-3.4% ngokulandelana, kanti izinga lokuthuthuka kwezinzwa lilonke lalingama-85.7% nama-71.4% ngokulandelana.Imiphumela emibi kakhulu yayiyisicanucanu (19.6% no-7.1%), ukubona izinto ezingekho (9.8% no-11.9%) kanye nesiyezi (13.7% no-7.1%).Imiphumela yalolu cwaningo iphinde yaqinisekisa ukusebenza nokuphepha kwe-ziconotide enconyiwe njengomjovo we-intrathecal womugqa wokuqala.

Ucwaningo lokuqala nge-ziconotide lungalandelelwa emuva kuma-1980s, lapho ukusetshenziswa kokwelapha okungaba khona kwama-peptide aqinile nanjengamaprotheni ku-conus venom kwahlolwa okokuqala.Lawa ma-conotoxins ama-peptide amancane acebile ngamabhondi e-disulfide, ngokuvamile izinsalela ze-10-40 ubude, ukuze aqondise iziteshi ze-ion ezihlukahlukene, i-GPCR kanye namaprotheni e-transporter ngokuphumelelayo nangokukhetha.I-Ziconotide iyi-25-peptide etholakala ku-Conus magus, equkethe izibopho ezintathu ze-disulfide, futhi i-β-fold yayo emfushane ihlelwe ngokwendawo ibe isakhiwo esiyingqayizivele se-dimensional emithathu, esivumela ukuthi ivimbele ngokukhetha iziteshi ze-CaV2.2.


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